Atosiban

(BAN, USAN, rINN)
Synonyms: Atosibaani; Atosibanum; ORF-22164; RWJ-22164. 1-(3-Mercaptopropionic acid)-2-[3-(p-ethoxyphenyl)nine-8ethyltyrosine),4
Cyrillic synonym: Атозибан.

💊 Chemical information

Chemical formula: C43H67N11O12S2 = 994.2.
CAS — 90779-69-4.
ATC — G02CX01.
ATC Vet — QG02C X01.

💊 Adverse Effects and Precautions

Adverse effects reported in women receiving atosiban for premature labour include nausea and vomiting, headache, dizziness, flushes, tachycardia, hypotension, hyperglycaemia, and injection site reactions. Atosiban should not be used where continuation of pregnancy is hazardous to mother or fetus, including where gestational age is below 24 or over 33 weeks, in eclampsia or severe pre-eclampsia, intra-uterine growth retardation and abnormal fetal heart rate, suspected intra-uterine infection, placenta praevia, or abruptio placentae. Monitoring of uterine contractions and fetal heart rate is recommended during use, and blood loss should be monitored after delivery. Although there has been some concern about fetal exposure, licensed product information states that no specific adverse effects on the newborn have been reported.

💊 Pharmacokinetics

In women in premature labour, atosiban reaches steady-state plasma concentrations within one hour of the start of infusion, and has a terminal half-life of 1.7 hours after stopping infusion. Atosiban is 46 to 48% bound to plasma proteins, and crosses the placenta. It is metabolised to an active metabolite, which is excreted in the urine; both atosiban and this metabolite are distributed into breast milk.

💊 Uses and Administration

Atosiban is a peptide analogue of oxytocin but with oxytocin antagonist properties. It is used as a tocolytic in the management of premature labour. Atosiban is given intravenously as the acetate, but doses are expressed in terms of the base. An initial bolus dose equivalent to atosiban 6.75 mg is given by intravenous injection (as a solution containing 7.5 mg/mL) over one minute. This is immediately followed by a continuous infusion of 300 micrograms/minute for 3 hours, then 100 micrograms/minute for up to 45 hours, as a solution containing 750 micrograms/mL. The total duration of treatment should not exceed 48 hours, and the total dose should not exceed 330 mg.

Premature labour.

References.
1. Romero R, et al. An oxytocin receptor antagonist (atosiban) in the treatment of preterm labor: a randomized, double-blind, placebo-controlled trial with tocolytic rescue. Am J Obstet Gynecol 2000; 182: 1173–83
2. Valenzuela GJ, et al. Maintenance treatment of preterm labor with the oxytocin antagonist atosiban: the Atosiban PTL-098 Study Group. Am J Obstet Gynecol 2000; 182: 1184–90
3. Moutquin JM, et al. Double-blind, randomized, controlled trial of atosiban and ritodrine in the treatment of preterm labor: a multicenter effectiveness and safety study. Am J Obstet Gynecol 2000; 182: 1191–9
4. The Worldwide Atosiban versus Beta-agonists Study Group. Effectiveness and safety of the oxytocin antagonist atosiban versus beta-adrenergic agonists in the treatment of preterm labour. Br J Obstet Gynaecol 2001; 108: 133–42
5. The European Atosiban Study Group. The oxytocin antagonist atosiban versus the beta-agonist terbutaline in the treatment of preterm labor: a randomized, double-blind, controlled study. Acta Obstet Gynecol Scand 2001; 80: 413–22
6. French/Australian Atosiban Investigators Group. Treatment of preterm labor with the oxytocin antagonist atosiban: a doubleblind, randomized, controlled comparison with salbutamol. Eur J Obstet Gynecol Reprod Biol 2001; 98: 177–85
7. Coomarasamy A, et al. Oxytocin antagonists for tocolysis in preterm labour—a systematic review. Med Sci Monit 2002; 8: RA268–73
8. Tsatsaris V, et al. Atosiban for preterm labour. Drugs 2004; 64: 375–82
9. Husslein P, et al. Atosiban versus usual care for the management of preterm labor. J Perinat Med 2007; 35: 305–13.

💊 Preparations

Proprietary Preparations

Arg.: Tractocile; Austria: Tractocile; Belg.: Tractocile; Braz.: Tractocile†; Cz.: Tractocile; Denm.: Tractocile; Fin.: Tractocile; Fr.: Tractocile; Ger.: Tractocile; Gr.: Tractocile; Hong Kong: Tractocile; Hung.: Tractocile; Irl.: Tractocile; Ital.: Tractocile; Malaysia: Tractocile; Mex.: Tractocile; Neth.: Tractocile; Norw.: Tractocile; NZ: Tractocile; Pol.: Tractocile; Port.: Tr ac tocile; S.Afr.: Tractocile; Spain: Tractocile; Swed.: Tractocile; Switz.: Tr actocile; UK: Tractocile.
Published October 11, 2018.